Liproxstatin-1 analog | CAS# 1170643-61-4 | Analog

MedKoo Cat#: 574096 | Name: Liproxstatin-1 analog

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Liproxstatin-1 analog is an analog of the ferroptosis inhibitor liproxstatin-1.

Chemical Structure

Liproxstatin-1 analog

CAS#1170643-61-4

Theoretical Analysis

MedKoo Cat#: 574096

Name: Liproxstatin-1 analog

CAS#: 1170643-61-4

Chemical Formula: C16H24N4

Exact Mass: 272.2001

Molecular Weight: 272.40

Elemental Analysis: C, 70.55; H, 8.88; N, 20.57

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 500.00	2 Weeks
10mg	USD 950.00	2 Weeks

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Synonym

Liproxstatin-1 analog

IUPAC/Chemical Name

N-(1,1-dimethylethyl)-spiro[piperidine-4,2′(1′H)-quinoxalin]-3′-amine

InChi Key

XSZONDARYJTXFE-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H24N4/c1-15(2,3)20-14-16(8-10-17-11-9-16)19-13-7-5-4-6-12(13)18-14/h4-7,17,19H,8-11H2,1-3H3,(H,18,20)

SMILES Code

CC(C)(C)NC1=NC2=CC=CC=C2NC13CCNCC3

Appearance

A crystalline solid

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Liproxstatin-1 is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC50=22 nM).

In vitro activity:

In order to test if Lip-1 (Liproxstatin-1) was able to protect HEI-OC1 cells from neomycin-induced ototoxicity, the cells were cotreated with Lip-1 and neomycin. Using CCK8 assay, it was confirmed that cell viability in the presence of Lip-1 was indeed significantly higher than in the absence of Lip-1 (Figure 2(d)). Next, to explore whether the protection mechanisms of Lip-1 are partly due to apoptosis, the apoptotic rate of HEI-OC1 cells was measured by flow cytometry. The results showed that the proportions of dead and apoptotic cells markedly increased in the neomycin group compared to the control group. Lip-1 remarkably decreased the cell death, while it had no significant effect on reducing the apoptotic cells (Supplemental Fig. 1A-C). In addition, Lip-1 reduced cell death induced by neomycin measured by TUNEL labeling (Supplemental Fig. 1D and E). Reference: Oxid Med Cell Longev. 2020 Dec 1;2020:1782659. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7725559/

In vivo activity:

Whether spinal cord ferroptosis contributes to morphine tolerance was investigated. C57BL/6 mice were continuously subcutaneously injected with morphine, with or without the ferroptosis inhibitor liproxstatin-1. Chronic morphine exposure led to morphine antinociception tolerance, accompanied by loss of spinal cord neurons, increase in the levels of iron, malondialdehyde, and reactive oxygen species, and decreases in the levels of superoxide dismutase. Additionally, inflammatory response and mitochondrial shrinkage, processes that are involved in ferroptosis, were observed. 10 mg/kg of liproxstatin-1 could alleviate iron overload by balancing transferrin receptor protein 1/ferroportin expression and attenuate morphine tolerance by increasing glutathione peroxidase 4 levels, while reducing the levels of malondialdehyde and reactive oxygen species. It also downregulated the expression of extracellularly regulated protein kinases that had been induced by chronic morphine exposure. These results indicate that spinal cord ferroptosis contributes to morphine tolerance, while liproxstatin-1 attenuates the development of morphine tolerance. Reference: ACS Chem Neurosci. 2019 Dec 18;10(12):4824-4833. https://pubs.acs.org/doi/10.1021/acschemneuro.9b00539

	Solvent	mg/mL	mM
Solubility
	DMF	25.0	91.78
	DMSO	15.0	55.07
	Ethanol	5.0	18.36

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 272.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zheng Z, Tang D, Zhao L, Li W, Han J, Hu B, Nie G, He Y. Liproxstatin-1 Protects Hair Cell-Like HEI-OC1 Cells and Cochlear Hair Cells against Neomycin Ototoxicity. Oxid Med Cell Longev. 2020 Dec 1;2020:1782659. doi: 10.1155/2020/1782659. PMID: 33343803; PMCID: PMC7725559. 2. Chen X, Zhang B, Liu T, Feng M, Zhang Y, Zhang C, Yao W, Wan L. Liproxstatin-1 Attenuates Morphine Tolerance through Inhibiting Spinal Ferroptosis-like Cell Death. ACS Chem Neurosci. 2019 Dec 18;10(12):4824-4833. doi: 10.1021/acschemneuro.9b00539. Epub 2019 Nov 14. PMID: 31682397.

In vitro protocol:

In vivo protocol:

1. Chen X, Zhang B, Liu T, Feng M, Zhang Y, Zhang C, Yao W, Wan L. Liproxstatin-1 Attenuates Morphine Tolerance through Inhibiting Spinal Ferroptosis-like Cell Death. ACS Chem Neurosci. 2019 Dec 18;10(12):4824-4833. doi: 10.1021/acschemneuro.9b00539. Epub 2019 Nov 14. PMID: 31682397.